Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis
Teriparatide acetate (TA), which directly promotes bone formation, is subcutaneously injected to treat osteoporosis. In this study, TA with a once-weekly administration regimen was loaded on dissolving microneedles (DMNs) to effectively deliver it to the systemic circulation via the transdermal rout...
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| Format: | Article |
| Language: | English |
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MDPI AG
2022-09-01
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| Series: | Polymers |
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| Online Access: | https://www.mdpi.com/2073-4360/14/19/4027 |
| _version_ | 1797477315641344000 |
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| author | Jeeho Sim Geonwoo Kang Huisuk Yang Mingyu Jang Youseong Kim Hyeri Ahn Minkyung Kim Hyungil Jung |
| author_facet | Jeeho Sim Geonwoo Kang Huisuk Yang Mingyu Jang Youseong Kim Hyeri Ahn Minkyung Kim Hyungil Jung |
| author_sort | Jeeho Sim |
| collection | DOAJ |
| description | Teriparatide acetate (TA), which directly promotes bone formation, is subcutaneously injected to treat osteoporosis. In this study, TA with a once-weekly administration regimen was loaded on dissolving microneedles (DMNs) to effectively deliver it to the systemic circulation via the transdermal route. TA activity reduction during the drying process of various TA polymer solutions formulated with hyaluronic acid and trehalose was monitored and homogeneities were assessed. TA-DMN patches fabricated using centrifugal lithography in a two-layered structure with dried pure hyaluronic acid on the base layer and dried TA polymer solution on the top layer were evaluated for their physical properties. Rhodamine-B-loaded TA-DMNs were found to form perforations when inserted into porcine skin using a shooting device. In addition, 87.6% of TA was delivered to the porcine skin after a 5-min TA-DMN patch application. The relative bioavailability of TA via subcutaneous injection was 66.9% in rats treated with TA-DMN patches. The maximal TA concentration in rat plasma was proportional to the number of patches used. Therefore, the TA-DMN patch fabricated in this study may aid in the effective delivery of TA in a patient-friendly manner and enhance medical efficacy in osteoporosis treatment. |
| first_indexed | 2024-03-09T21:15:50Z |
| format | Article |
| id | doaj.art-54e8ab77b4a34b8eb7b25cd0a926c4d0 |
| institution | Directory Open Access Journal |
| issn | 2073-4360 |
| language | English |
| last_indexed | 2024-03-09T21:15:50Z |
| publishDate | 2022-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Polymers |
| spelling | doaj.art-54e8ab77b4a34b8eb7b25cd0a926c4d02023-11-23T21:33:03ZengMDPI AGPolymers2073-43602022-09-011419402710.3390/polym14194027Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of OsteoporosisJeeho Sim0Geonwoo Kang1Huisuk Yang2Mingyu Jang3Youseong Kim4Hyeri Ahn5Minkyung Kim6Hyungil Jung7Department of Biotechnology, Yonsei University, Seoul 03722, KoreaDepartment of Biotechnology, Yonsei University, Seoul 03722, KoreaJUVIC Inc., No. 208, Digital-ro 272, Guro-gu, Seoul 08389, KoreaJUVIC Inc., No. 208, Digital-ro 272, Guro-gu, Seoul 08389, KoreaDepartment of Biotechnology, Yonsei University, Seoul 03722, KoreaDepartment of Biotechnology, Yonsei University, Seoul 03722, KoreaDepartment of Biotechnology, Yonsei University, Seoul 03722, KoreaDepartment of Biotechnology, Yonsei University, Seoul 03722, KoreaTeriparatide acetate (TA), which directly promotes bone formation, is subcutaneously injected to treat osteoporosis. In this study, TA with a once-weekly administration regimen was loaded on dissolving microneedles (DMNs) to effectively deliver it to the systemic circulation via the transdermal route. TA activity reduction during the drying process of various TA polymer solutions formulated with hyaluronic acid and trehalose was monitored and homogeneities were assessed. TA-DMN patches fabricated using centrifugal lithography in a two-layered structure with dried pure hyaluronic acid on the base layer and dried TA polymer solution on the top layer were evaluated for their physical properties. Rhodamine-B-loaded TA-DMNs were found to form perforations when inserted into porcine skin using a shooting device. In addition, 87.6% of TA was delivered to the porcine skin after a 5-min TA-DMN patch application. The relative bioavailability of TA via subcutaneous injection was 66.9% in rats treated with TA-DMN patches. The maximal TA concentration in rat plasma was proportional to the number of patches used. Therefore, the TA-DMN patch fabricated in this study may aid in the effective delivery of TA in a patient-friendly manner and enhance medical efficacy in osteoporosis treatment.https://www.mdpi.com/2073-4360/14/19/4027osteoporosisdissolving microneedleteriparatide acetatetrehalosecentrifugal lithographypharmacokinetic profile |
| spellingShingle | Jeeho Sim Geonwoo Kang Huisuk Yang Mingyu Jang Youseong Kim Hyeri Ahn Minkyung Kim Hyungil Jung Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis Polymers osteoporosis dissolving microneedle teriparatide acetate trehalose centrifugal lithography pharmacokinetic profile |
| title | Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis |
| title_full | Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis |
| title_fullStr | Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis |
| title_full_unstemmed | Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis |
| title_short | Development of Clinical Weekly-Dose Teriparatide Acetate Encapsulated Dissolving Microneedle Patch for Efficient Treatment of Osteoporosis |
| title_sort | development of clinical weekly dose teriparatide acetate encapsulated dissolving microneedle patch for efficient treatment of osteoporosis |
| topic | osteoporosis dissolving microneedle teriparatide acetate trehalose centrifugal lithography pharmacokinetic profile |
| url | https://www.mdpi.com/2073-4360/14/19/4027 |
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